In modern pharmaceuticals, fluoroquinolone antibiotics belong to an independent group of drugs obtained as a result of chemical synthesis and having a wide spectrum of action. They are characterized by high pharmacokinetic properties and excellent ability to penetrate cells and tissues, including the membranes of bacteria and macroorganisms.
Currently, all fluoroquinolones are divided into 4 main groups, which determine their properties and characteristics.
The sequence of development of new drugs is the basis for their division into groups. Thus, fluoroquinolones of the 1st, 2nd, 3rd and 4th generations are known.
The first drugs were developed in the 60s of the last century. Nalidixic acid (active ingredient) of antibiotics and its constituents (oxolinic and pipemidic acids) have shown good results in the fight against bacteria that cause uncomplicated pathologies of the urinary tract and intestines (dysentery, enterocolitis).
The following drugs belong to the first generation: Negram, Nevigramon - drugs based on nalidixic acid. They have a negative effect on bacteria of the following types: Proteus, Salmonella, Shigella, Klebsiella.
Despite their high efficiency, these funds are characterized by reduced bio-permeability and a large number of side effects. Thus, numerous studies have shown one hundred percent resistance to antibiotics of bacteria such as gram-positive cocci, anaerobes and Pseudomonas aeruginosa.
When taking the drugs, the patients complained of dyspeptic disorders, hemolytic anemia, overexcitation of the nervous system and cytopenia. In addition, the peculiarities of the effects of drugs prohibit taking them in acute pyelonephritis and renal failure.
But since antibiotics of this group were recognized as a very promising direction, research and development of new drugs did not stop. Twenty years after the appearance of nalidixic acid, fluoroquinolone antimicrobial agents, DNA gyrase inhibitors, were synthesized.
Second generation drugs
Fundamentally new substances were obtained by introducing fluorine atoms into quinoline molecules. Due to this compound, they got their name - fluoroquinolones. The bactericidal efficiency and characteristics of the drugs completely depend on the number of fluorine atoms (one or more) and their location in different positions of the quinoline atoms.
Second generation fluoroquinolones have shown a number of advantages over pure quinolones.
A breakthrough in pharmaceuticals was the ability of drugs to comprehensively affect the following types of bacteria:
- gram-negative cocci and bacilli (salmonella, protea, shigella, enterobacteria, serrations, citrobacters, meningococci, gonococci, etc.);
- gram-positive bacilli (corynebacteria, listeria, anthrax pathogens);
- staphylococci;
- legionella;
- in some cases, tubercle bacillus.
Second-generation fluoroquinolones include:
- Ciprofloxacin (Tsiprinol and Tsiprobay), called the gold standard in this group of medicines. The drug is widely used in the treatment of infections of the lower respiratory tract (nosocomial pneumonia and chronic bronchitis), urinary system and intestines (salmonellosis, shigellosis). Also, the list of pathologies to be cured with this drug includes infectious diseases such as prostatitis, sepsis, tuberculosis, gonorrhea, anthrax.
- Norfloxacin (Nolitsin), which creates the maximum concentration of active substances in the urinary system and gastrointestinal tract. Indications for use are infections of the genitourinary system and intestines, prostatitis, gonorrhea.
- Ofloxacin (Tarivid, Ofloxin) is the most effective agent among second-generation fluoroquinolones against chlamydia and pneumococci. Its effect on anaerobic bacteria is slightly worse. It is prescribed for the treatment of infections of the lower respiratory and urinary tract, with the prostate, intestinal pathologies, gonorrhea, tuberculosis, severe infections of the pelvic organs, skin, joints, bones and soft tissues.
- Pefloxacin (Abaktal) is somewhat inferior in efficiency to the above-described drugs, but better than others it penetrates the biological membranes of bacteria. It is used for the same pathologies as other fluoroquinolone antibiotics, including secondary bacterial meningitis.
- Lomefloxacin (Maxaquin) does not act on anaerobic infection and shows low results when interacting with pneumococci, but differs in the level of bioavailability reaching 100%. In Russia, it is used to treat chronic bronchitis, genitourinary infections and tuberculosis (in combination therapy).
Preparations from the group of fluoroquinolones have taken leading positions in the treatment of pathologies caused by bacterial infection. Their main advantages up to the present day are:
- high level of bioactivity;
- a unique mechanism of action that is not used by any other drug for this purpose;
- excellent penetration through the membranes of bacteria and the ability to create protective substances in the cell, in concentration close to serums;
- good patient tolerance.
Third and fourth generation drugs
Despite the fact that the main goal of developments aimed at expanding the spectrum of action of antibiotics of this group and increasing the level of solubility of compounds acting on especially dangerous macroorganisms (including anaerobes) was achieved as a result of the creation of second generation quinolones, the research did not stop. Soon, drugs of the third and fourth generations appeared.
The third generation fluoroquinolones include the drug Levofloxacin (Tavanic), which is the levorotatory isomer of Ofloxacin. In pharmacology, it is defined as a respiratory quinolone, which differs from its predecessors by a higher activity against pneumococci (including strains resistant to penicillin drugs). The bioavailability of the drug is equal to 100%.
Levofloxacin is recommended for use in infectious lesions of the upper (acute sinusitis) and lower respiratory (pneumonia, chronic bronchitis) tract, with inflammation of the urinary system, skin and soft tissues. Effective in the treatment of anthrax.
The fourth generation drug is Moxifloxacin (Avelox), which has a more effective effect on pneumococci (including those resistant to macrolides and penicillins) and atypical pathogenic microorganisms (mycoplasma, chlamydia, etc.).
Unlike almost all drugs in this group, it successfully fights non-spore-forming anaerobic bacteria. But at the same time, it is inferior in effectiveness against Pseudomonas aeruginosa and gram-negative bacteria of the intestinal series. Indications for the use of the drug are acute sinusitis, pneumonia, chronic bronchitis, infectious lesions of soft tissues and skin.
Medicines of both the first and subsequent generations have peculiarities of chemical structure and physical properties, which seriously complicates the task of manufacturing preparations in an injectable form. Until now, it has not been possible to obtain sufficiently stable solutions for intravenous administration. This is what determines the fact that almost all names of fluoroquinolones are available only in the form of tablets for oral use.
There are several names of antibiotics of this group, produced in the form of solutions (including Enrofloxacin), which are highly valued by scientists.
They provide an opportunity to develop new drugs. So, today dosage forms for topical use are produced, in which fluoroquinolones are presented in the form of ear or eye drops and ointment.
According to researchers from all countries, fluoroquinolones are the future of all antibacterial pharmaceuticals.
Antibiotics fluoroquinolones are represented by a fairly extensive group of medications that have antibacterial activity against different groups of pathogenic microorganisms. The list of drugs related to these antibiotics is extensive, including many highly effective drugs.
In the external environment, a person daily encounters a large number of pathogens. A significant part lives directly inside, some are useful, others, under certain circumstances, cause this or that disease.
Fluoroquinolones are represented by a wide group of drugs that have a wide spectrum of action, destroy a variety of microbes when they enter the body. The concept of funds was formed back in the 60s. last century. Since then, scientists have done a lot of research and developed safer drugs than those used about 50 years ago.
Mechanism of action
Fluoroquinolones (the list of drugs includes agents with varying degrees of effectiveness) have a detrimental effect on gram-positive and gram-negative types of bacteria. They quickly destroy Pseudomonas aeruginosa, staphylococci and streptococci. High efficiency is noted in the fight against shigella, gonococci and pneumococci.
Additionally, fluoroquinolones are allowed to be used in the fight against bacilli of various types, chlamydia and tubercle bacillus. The drugs are not able to completely destroy the last type of microorganisms, but are used as an auxiliary element of complex therapy.
The mechanism of action of medicines is due to the sequence of several processes:
- After penetration into the body, the components of tablets or other dosage forms are quickly distributed throughout all organs and systems, freely penetrate into different cells, ensuring high efficiency.
- Further, substances are concentrated in the area of inflammation, after which they suppress the synthesis of DNA molecules in cells that provoke the disease.
- Additionally, fluoroquinolones disrupt metabolic processes in them, which leads to a violation of the process of reproduction and spread to healthy areas.
- Thanks to these mechanisms, a rather rapid death of microbes of various types occurs, and the regeneration process starts.
It is worth noting that the active substances in the composition of one or another agent have a pronounced effect precisely due to the rapid penetration into all tissues of the body. They easily pass the placental barrier, so they can be dangerous for women during pregnancy.
The advantage of drugs in this group is also considered to be high bioavailability, because the maximum concentration of active ingredients is reached within 3 hours after ingestion and lasts for a long time. Due to the slow elimination after the end of the course of antibiotic therapy, the activity of the drugs decreases gradually.
Classification: four generations
To date, experts identify 4 generations of fluoroquinolones. Each of them is effective against different groups of microorganisms.
Non-fluorinated quinolones
Fluoroquinolones (the list of drugs is extensive, allows you to choose a suitable agent in each case) of the first generation are called non-fluorinated. This is the very first group of drugs, which includes various drugs used to treat patients today. The active components of any product are obtained by processing nalidixic, oxolinic, pipemidic acid.
They are completely synthetic drugs, but they have a rather narrow spectrum of action. They are actively used in the treatment of diseases of the urinary system, since they are excreted unchanged, providing a pronounced therapeutic effect. Another advantage of the drugs is a high concentration in the patient's blood, as well as in some organs, for example, the bladder, intestines.
However, non-fluorinated quinolones are almost unable to penetrate the cells of the liver, lungs and other organs, so the area of their use is narrow, in contrast to the means of the next generations. In addition, they provoke many side reactions even when used correctly.
The following drugs belong to the first generation of fluoroquinolones: Nevigramon, Palin, Negram and others.
Gram-negative
The second generation of antibiotics in this group is called gram-negative, since they are active mainly against gram-microorganisms. The study and research of the drugs lasted about 20 years, after which the first antibiotic of this generation, Norfloxacin, was developed.
They got it by attaching a fluorine atom to a specific molecule. Unlike non-fluorinated antibiotics, gram-negative fluoroquinolones have the ability to quickly penetrate into the cells of almost all internal organs and concentrate in them. This ensures high efficiency and responsiveness.
A great advantage of gram-negative antibiotics is their high activity against Staphylococcus aureus. This microorganism provokes rather dangerous diseases and, if untreated, the patient's condition deteriorates greatly, there is a danger to life.
The most popular member of this generation today is Ciprfloxacin. It is very effective in combating diseases of the respiratory, digestive, reproductive and urinary systems. Among the disadvantages are pronounced side effects from the central nervous system, digestive organs.
Respiratory
Fluoroquinolones from 3 generations were called respiratory. The list of drugs includes Levofloxacin, Temafloxacin and others. This group got its name because of the high effectiveness of drugs in the treatment of diseases of the upper and lower respiratory tract.
Many microorganisms that provoke sinusitis, sinusitis, bronchitis and pneumonia are very resistant to antibiotics from the penicillin group. Several decades ago, only they were used massively for the therapy of children and adults.
But with the advent of respiratory fluoroquinolones, the number of deaths from advanced pneumonia and bronchitis has decreased significantly, since they destroy even those microorganisms that are highly resistant to other antibiotics. Medicines are used not only to treat respiratory diseases, but also to eliminate the symptoms of infectious conditions.
The bioavailability of any 3rd generation product is close to 100%, which is also considered an advantage. Among the disadvantages, it is worth highlighting a high concentration not only in the affected, but also in healthy tissues. Active substances penetrate very quickly into the cells of organs, which does not allow their use for the treatment of pregnant and lactating women.
Respiratory anti-anaerobic
The mechanism of action of respiratory anti-anaerobic fluoroquinolones is almost the same as the drugs presented in the previous generation. They are also effective against pneumococci, staphylococci and streptococci, which are resistant to penicillins and even macrolides.
The latter are considered one of the most effective antibiotics, but even they are not always able to cope with bacteria.
Due to the wide spectrum of action and the rapid achievement of the therapeutic effect, the drugs are actively used in the treatment of bronchitis, otitis media, sinusitis. They are also effective for sinusitis, pneumonia of varying severity and even an unreleased form of tuberculosis.
High bioavailability, approaching absolute, helps to achieve a therapeutic result in a short time and with the use of minimum dosages of the drug.
However, the concentration of large doses of active substances in healthy tissues can provoke intoxication. Some drugs from this generation have recently been discontinued and are not used in treatment precisely because of their high toxicity.
Indications for use in the fields of medicine
The drugs of the fluoroquinolone group are actively used in various fields of medicine. In some cases, they are used as the main method of treatment, in others, as an auxiliary one.
Gastroenterology
Even the first generation of fluoroquinolones was actively used as the main treatment for inflammatory bowel diseases. The patient could get rid of acute symptoms of colitis, enteritis or enterocolitis in a few days. The course of treatment then lasted at least 2 weeks, but improvement was noted as early as 4-5 days after the start of admission.
As the pharmaceutical industry progressed, more improved drugs appeared, and their field of application expanded. For cholecystitis, bacterial gastritis, peptic ulcer disease, fluoroquinolones began to be used, which helped to suppress the activity of pathogenic microflora.
As the main method of treatment, drugs are not prescribed, since a whole range of funds is needed. But thanks to such antibiotics, the risk of complications is minimized.
Venereology and gynecology
Chlamydia, mycoplasmosis, gonorrhea and some other diseases are successfully treated with fluoroquinolones. At the same time, antibiotics are almost always the only treatment method, which excludes the likelihood of complications from the use of several medicines of different groups at once.
In gynecology, drugs are also actively used for endometritis, salpingitis, adnexitis. Bacterial vaginitis also responds well to 2nd and 3rd generation fluoroquinolones.
Dermatology
In the treatment of infected wounds, trophic ulcers and other diseases of the skin, preparations of the 2nd, 3rd and 4th generations are actively used. In most cases, they are prescribed topically in the form of ointments and creams, since they help to destroy bacteria directly in the lesion.
However, with extensive injuries and infection of lesions, specialists decide on the appointment of systemic agents in the form of tablets or injections. For a long time, scientists could not get the second form, but with its appearance, the scope of the drug has expanded.
Otolaryngology
Fluoroquinolones (the list of drugs has increased in the past few years) 3 generations are actively used in the treatment of any diseases of the upper and lower respiratory tract of an inflammatory nature. This is due to the high efficacy of respiratory antibiotics against pneumococci, streptococci, staphylococci.
It is worth noting that in the treatment of bronchitis, sinusitis, sinusitis, drugs from the penicillin group are often used in the initial stages. After 7-10 days of ineffective treatment, the specialist decides on the appointment of fluoroquinolones. In the past few years, many doctors have used this group of medicines immediately, shortening the treatment period and preventing complications.
Ophthalmology
For the prevention and treatment of postoperative complications from the visual apparatus, drops and ointments containing antibacterial components from the group of fluoroquinolones are actively used.
Means of the 2nd, 3rd and 4th generations are highly effective in the fight against keratitis, bacterial conjunctivitis. At the same time, drugs are not addictive, rarely provoke complications and almost always help to completely cure the disease.
Pulmonology
For any diseases of the lungs, pulmonologists quite often prescribe fluoroquinolones, especially the 2nd and 3rd generations. It is these drugs that quickly destroy pneumococci, streptococci, staphylococci, and sometimes help suppress the activity of the tubercle bacillus.
3rd generation fluoroquinolones such as Levofloxacin are used in pulmonology. Due to their effectiveness, fluoroquinolones can be used in the complex treatment of acute and chronic tuberculosis. As the main method, they are used to eliminate the symptoms of bronchitis, sinusitis, sinusitis of varying severity.
Urology and Nephrology
In urological practice, specialists also use antibiotics of this group. The first generation of non-fluorinated quinolones is suitable for the treatment of cystitis, urethritis in men and women. These medicines are concentrated in the organs of the urinary system, which helps to quickly achieve a therapeutic effect.
For pyelonephritis, glomerulonephritis, duct inflammation, or other kidney disease, nephrologists may use fluoroquinolones as pills or injections.
Fluoroquinolone antibiotics
Fluoroquinolones have a fairly large list of drugs. However, each generation has one or more of the most commonly used tools.
| Name of the drug | Description and action |
| Nevigramon | Available in capsule form. The composition contains nalidixic acid. The agent belongs to non-fluorinated quinolones, has a bacteriostatic and bactericidal effect. When it enters the body, it stops the development of pathogens, which leads to their gradual death. The drug is used mainly for the treatment of diseases of the urinary system. |
| Levofloxacin | It belongs to the 3rd generation fluoroquinolone group. Contains the active ingredient of the same name. It has a pronounced effect on microorganisms, quickly destroys streptococci, staphylococci, pneumococci and other bacteria. Effective in diseases of the respiratory, urinary, reproductive system. |
| Ciprofloxacin | Antibiotic from the group of gram-negative fluoroquinolones. It has a pronounced effect, is active against gram-negative and gram-positive bacteria, bacilli and even gonococci. Suppresses the development of microorganisms and leads to rapid death. The only drawback is the high risk of developing adverse reactions if instructions are violated. |
| Abaktal | Antibacterial drug of the 2nd generation, containing pefloxacin as an active ingredient. When ingested, it quickly concentrates in the affected area, destroys bacteria and prevents their spread to healthy areas. It is produced in tablet form, as well as in the form of a lyophilisate for solution preparation. |
| Floxal | The drug is from the group of fluoroquinolones of the 2nd generation. Contains ofloxacin as an active ingredient. Effectively copes with gram-positive and gram-negative pathogens. Available in eye drops and ointment. Most often used in the treatment of ophthalmic diseases. |
| Lomacin | Antimicrobial agent from the group of gram-negative fluoroquinolones, available in the form of tablets. The composition contains lomefloxacin. The substance has a pronounced effect, quickly suppresses the vital activity of bacteria and destroys them. |
| Vigamox | A 4-generation drug of fluoroquinolones, developed specifically for the treatment of eye diseases of bacterial origin. Available as drops. Moxifloxacin is present as an active ingredient. Upon contact with the mucous membrane, the component is rapidly absorbed and begins to act. |
Such means are used quite often. However, there are other highly effective medicines in the group. In each case, the specialist selects the necessary drug.
Possible side effects
When using fluoroquinolones of any generation, negative reactions may develop. Most often, complications arise when instructions are violated, but they can also appear under other circumstances.
The most common side effects are:
- Sleep disturbance (insomnia or drowsiness).
- Inability to concentrate on any subject.
- Decreased performance, weakness, fatigue.
- Loss of appetite, nausea and vomiting that does not bring relief.
- Pain in the stomach, intestinal colic.
- Frequent loose stools, increased gas production.
- Itching and irritation of the skin, the appearance of blisters filled with a clear or cloudy liquid.
- Increased salivation, lacrimation.
- Apathy, depression.
- Headache, dizziness.
Quincke's edema is considered the most severe complication of long-term uncontrolled intake of antibiotics of this group. In this case, the patient not only develops allergy symptoms, but also swelling of the mucous throat is observed, which can lead to suffocation. To prevent such complications, it is recommended that if complications appear, immediately stop taking it and consult a specialist.
Special instructions for admission
Experts insist on observing some rules that facilitate the treatment process and minimize the risk of complications:
- It is necessary to use drugs strictly according to the scheme and in the dosage prescribed by the doctor. Exceeding or decreasing the dose may worsen the general condition.
- You should strictly adhere to the doctor's recommendations and not prolong the course yourself.
- It is also forbidden to stop taking it earlier than the due date, since the antibiotic may not destroy all the germs, but if it is reappointed it will be ineffective.
- The tablets should be taken after meals in order to minimize negative reactions from the stomach and intestines.
- It is recommended to combine the course of antibiotic therapy with taking medications to normalize the intestinal microflora. Linex or Bifiform is suitable for this.
- It is strongly recommended not to drink alcohol during treatment. After the end of the course, it is worth adhering to this for another 2 weeks, which will reduce the load on the liver cells.
- When using external forms of the drug, you should first check your sensitivity to the drug. The duration of the course, as with the use of other forms, should not exceed the recommended one.
- If there is no effect of treatment for 10 days or if the condition worsens, you should consult a doctor. Perhaps the drug is not suitable for the patient and a different one is required.
If the patient has already taken any medication and considers it effective, doctors do not allow repeated treatment without a preliminary examination. The decision to prescribe drugs for children is made only by the pediatrician after examining the child.
Effective broad-spectrum antibiotics, fluoroquinolones, can quickly treat many diseases. The list of drugs is updated annually, so you can choose the right remedy for each patient.
Article design: Lozinsky Oleg
Video about fluoroquinolones
Fluoroquinolones - mechanisms of action and resistance:
What should a doctor do if his patient is allergic to antibiotics? Until recently, this question has baffled almost every therapist. Since the 60s of the last century, the answer has been found: quinolones. In modern medicine, drugs are used based on their derivatives - fluoroquinolones. How they work and how they differ from antibiotics will be discussed in the article below.
What are fluoroquinolones
This is a group of medicines with a pronounced antimicrobial effect. Medicines in this category are used as antibiotics with a wide range of uses. Moreover, these substances are not antibiotics in the full sense of the word. They have no natural analogue and differ from them in their structure.
A feature of fluoroquinolones is the presence of a fluorine atom in the structure. Hence the name of the group. The second distinguishing feature in the structures is the presence of a piperazine ring.
Fluoroquinolones are called second generation quinolones. Compared to their predecessors, fluoroquinolones are highly active.
Classification
Fluoroquinolones are classified by generation:
- 1st generation: nalidixic and oxolinic acids. Refers to non-fluorinated quinolones.
- 2nd generation: ofloxacin, norfloxacin, lomefloxacin, ciprofloxacin. Gram-negative substances.
- III generation: sparfloxacin, levofloxacin, and gatifloxacin. Respiratory fluoroquinolones.
- IV generation: gemifloxacin and moxifloxacin. They belong to the category of anti-anaerobic and respiratory substances.
List of drugs
Gatifloxacin
According to the list of fluoroquinolone drugs by generations, this substance belongs to the 4th generation. Release form: tablets and solution. Main substance: gatifloxacin. Indications for use: acute forms of otitis media and sinusitis, gonorrhea, pneumonia, infections of joints, skin and bones, bronchitis, cystic fibrosis.
Contraindications: minor children, pregnancy, drug allergy.
Side effects: fever, sweating, tachycardia, gastrointestinal disorders, arrhythmia, hematuria, visual impairment.
Analogs: Gatispan, Tekvin, Tabris, Zarquin, Gatimak, Gatigem, Zikvin.
Hemifloxacin
A pharmacological drug with this name is not officially registered. Hemifloxacin is the name of the active ingredient in many medicines. Indications for use: infectious diseases, exacerbation of chronic bronchitis, sinusitis in the acute stage.
Contraindications: hypersensitivity to the substance, pregnancy and lactation, an increase in the QT interval on the electrocardiogram, age up to 18 years.
Side effects: allergic reactions, disorder of the central nervous system (dizziness, tremors of the extremities, fear), changes in the functioning of the sensory organs, renal failure.
A preparation containing gemifloxacin: pills Faktiv.
Grepafloxacin
This active ingredient is available in preparations under various trade names. Indications for use: pneumonia (including atypical), gonorrhea, exacerbation of bronchitis, cervicitis and urethritis.
Contraindications: epilepsy, conditions predisposing to heart rhythm disturbances, pregnancy and lactation, allergies, age less than 18 years.
Side effects: allergies, dizziness, panic and fear, disturbances in the functioning of the organs of vision, hearing and taste, vomiting, loss of appetite, constipation.
Preparation containing grepafloxacin: Raksar.
Levofloxacin
An antibacterial drug from the group of fluoroquinolones, belonging to the 3rd generation. Active ingredient: levofloxacin. Release form: tablets, eye drops, injection solution.
Indications for use: tablets are used to treat infectious diseases of the upper and lower respiratory tract, prostatitis, skin and urinary tract infections, bacteremia. Eye drops are used to treat eye infections. The solution is used to treat infections of the upper and lower respiratory tract, ENT organs.
Contraindications: pregnancy and lactation, renal failure, age up to 18 years, epilepsy.
Side effects: diarrhea, increased activity of liver enzymes, nausea.
Analogs:
- for drops - Tsipromed, Ophthalmol;
- for tablets - Xenaquin, Sparflo, Levoflox, Remedy, Haileflox, Tanflomed, Maklevo, Lefoktsin, Glevo;
- for solution - Basidzhen, Tsipronat, Leflobakt.
Lomefloxacin
A Russian drug based on an active substance - lomefloxacin. Release form: tablets. Indications: osteomyelitis, infections of the gastrointestinal tract, respiratory organs, skin, urinary and biliary tract, as well as for gonorrhea and chlamydia.
Contraindications: age up to 18 years, pregnancy and lactation, allergy to the drug.
Side effects: cough, bronchospasm, gastrointestinal tract disorders, vasculitis, back and joint pain, disorders in the central nervous system, cardiovascular and genitourinary systems, allergic reactions.
Analogs: Abaktal, Quintor, Pefloxacin, Maksaquin, Lofox, Lomatsin, Xenaquin, Lomflox.
Moxifloxacin
Active ingredient: moxifloxacin. Release form: tablets. Indications for use: urogenital infections, upper or lower respiratory tract infections, skin infections. The complex is used for the treatment of tuberculosis.
Contraindications: tendency to seizures, liver failure, allergies, pseudomembranous colitis, age up to 18 years, pregnancy.
Side effects: anemia, gastrointestinal tract disorders, hyperglycemia, tachycardia, shortness of breath, hallucinations, convulsions.
Analogs: Avelox, Moxie Fluor 400, Tevalox, Plevilox, Moximak, Moxin and Vigamox.
Nalidixic acid
The active substance - nalidixic acid - is a part of many drugs. Indications for use: cystitis, pyelitis, pyelonephritis, cholecystitis, otitis media.
Contraindications: oppression of the respiratory center, impaired liver function, the first trimester of pregnancy, age up to 2 years.
Side effects: vomiting, nausea, diarrhea, allergic reactions.
Nevigramon, Cistidix, Nilidixan, Nogram, Urodiksin, Vintomilon, Negram. The release is carried out in tablets or capsules.
Norfloxacin
Release form: eye and ear drops, tablets. Active ingredient: norfloxacin. Indications: used for infections of bacterial origin of the urinary tract, reproductive system, gastrointestinal tract, for gonorrhea and travelers' diarrhea.
Contraindications: age up to 18 years, pregnancy and lactation, intolerance to the components.
Side effects: nausea, abdominal pain, diarrhea, vomiting, urethral bleeding, dizziness, headache, tachycardia, tremor, arthralgia.
Analogs: Nolitsin, Norilet, Normaks, Sophazin, Chibroxin, Norbactin, Yutybid, Norfatsin, Noroxin, Renor.
Oxolinic acid
The acid is part of antimicrobial drugs. Active substance: oxolinic acid. Indications for the use of fluoroquinolone: prostatitis, pyelonephritis, pyelitis, prevention of infection during instrumental studies (for example, catheterization).
Contraindications: pregnancy, lactation, renal or hepatic failure, epilepsy, allergies, age up to 2 years, old age.
Side effects: disorders of the gastrointestinal tract, allergic reactions, general weakness, dizziness, visual impairment, photosensitivity.
Acidic preparations: Dioxacin and Gramurin (available in tablets).
Ofloxacin
One of the respiratory drugs is fluoroquinolones. Release form: ointment, tablets, solutions for infusion (drops). Active ingredient: ofloxacin. Indications for use: diseases of the ENT organs, infections of the urinary tract and kidneys, pneumonia, chlamydia, prostatitis, gonorrhea, conjunctivitis, blepharitis and others.
Contraindications: pregnancy, lactation, age up to 18 years, epilepsy, allergies.
Side effects: nausea, vomiting, flatulence, decreased appetite, diarrhea.
Analogs:
- tablets - Zanocin, Ofloxin, Oflocid, Glaufos, Zoflox;
- solutions - Tarivid, Oflo;
- ointment - Floxal (eye);
- drops for eyes and ears - Dancil and Uniflox.
Pefloxacin
Domestic antimicrobial medication. Active ingredient: pefloxacin. Release form: solution, tablets. Indications: typhoid fever, sepsis, prostatitis, gonorrhea, cholecystitis, eye infections, middle ear infections, pharyngeal and laryngeal infections.
Contraindications: hemolytic anemia, epilepsy, pregnancy and breastfeeding, allergies, age up to 18 years.
Side effects: headaches, fatigue, diarrhea, flatulence, dysuria, edema (allergic, including Quincke's edema), tachycardia and others.
Analogs: Leflocin, Perti, Pelox-400, Unicpef, Pefloxabol.
Pipemidic acid
Release form: capsules, tablets, vaginal suppositories, suspension (for children). Active ingredient: pipemidic acid. Indications for use: urinary tract infections (diseases in acute or chronic form).
Contraindications: pregnancy, renal failure.
Side effects: allergic skin reactions, nausea, photosensitivity, abdominal pain.
Analogs: Balurol, Naril, Pipefort, Pimidel, Pipem, Palin.
Sparflo
Active ingredient: Sparfloxacin is a poorly soluble substance of the fluoroquinolone group, which has an antibacterial orientation. Release form: tableted. Indications: prostatitis, diseases of the genital organs, infections of the ENT organs, infections of the abdominal cavity, sepsis, skin infections, leprosy, gonorrhea.
Contraindications: epilepsy, tendency to change the heart rate, pregnancy and lactation, renal failure, age up to 18 years, allergies.
Side effects: headaches, tremors, seizures, fear, shortness of breath, vomiting, fever, hyperglycemia, hot flashes, hepatitis and others.
Ciprofloxacin
Active ingredient: ciprofloxacin. Release form: drops (for eyes and ears), tablets. Indications for use: blepharitis, keratitis, barley, infections brought into the eye by foreign bodies, conjunctivitis, otitis media - for drops. Tablets are prescribed for diseases of the otolaryngological organs and for respiratory tract infections, prostatitis, pyelonephritis, cystitis, peritonitis, sepsis.
Contraindications: viral keratitis, allergies. Eye drops should not be used for children under one year old. For tablets: pregnancy and lactation, renal failure, epilepsy, under 18 years of age.
Side effects: itching, slight burning sensation, lacrimation, decreased vision or hearing, the appearance of white blotches in patients with ulcerative eye lesions, allergic reactions. For tablets - disorders of the gastrointestinal tract, allergic reactions, dysfunction of the central nervous system.
Analogs: Tsifran, Tsipromed, Sifloks, Floksimed, Tsipro, Tsiprinol, Mikrofloks, Recipro, Tseprova, Quintor.
Indications
Preparations of the fluoroquinolone group are used in cases where conventional antibiotics cannot cope:
- anthrax;
- typhoid fever;
- pneumonia and bronchitis;
- gonorrhea;
- salmonellosis;
- pyelonephritis;
- chlamydia;
- dysentery;
- cystitis.
Fluoroquinolones are widely used in gynecology, urology (for example, for prostatitis), ophthalmology, otolaryngology and other fields of medicine.
Mechanism of action
In clinical trials, it was found that fluoroquinolones, unlike conventional antibiotics, do not weaken harmful bacteria, but kill them. This happens by the penetration of an active substance into the structure of a harmful microorganism and stopping the process of cell reproduction.
Fluoroquinolones penetrate the body faster. For several hours, substances enter all tissues or liquids. After passing through all systems of the human body, drugs leave it through the urinary tract.
Application methods
When taking drugs in this group, it is important to understand that they are more likely to cause side effects if taken incorrectly than antibiotics.
The frequency, dose and duration of the course is determined by the doctor. It is worth strictly following his recommendations and maintaining equal intervals between doses. If the appointment is missed, a single dose should be taken as soon as possible. But do not do this when the next reception is approaching. It is strictly forbidden to double the dose. The tablets are taken with a sufficient amount of water.
It is worth adjusting the course of taking fluoroquinolones if other drugs are prescribed in the complex. This is best done in case additional medications interact negatively with fluoroquinolones.
Contraindications
Medicines from the fluoroquinolone class are generally safe, but they have their own contraindications:
- pediatric diseases (all drugs are not used in children under 2 years of age, some are limited to 18 years);
- pregnancy and lactation;
- allergy to quinolone substances.
Side effects
Negative effects are less common than with antibiotics, but if taken incorrectly, they appear much more often:
- disorders of the gastrointestinal tract (nausea, diarrhea, vomiting);
- tachycardia, arrhythmia;
- disturbances in the functioning of the sense organs (vision, smell, taste);
- unstable work of the central nervous system (dizziness, headaches, tremors, convulsions);
- fungus on the mucous membranes of the genitals and mouth;
- tendon rupture, inflammation of the cartilage tissue;
- sleep disturbance;
- periodic pain in the muscles;
- nephritis;
- painful photosensitivity;
- allergic reactions (itching, hives, swelling);
- pseudomembranous colitis (rarely appears, only against the background of severe dysbiosis or intestinal clostridial damage).
Fluoroquinolone antibiotics are antibacterial agents obtained by chemical synthesis that can suppress the activity of gram-positive and gram-negative microorganisms. They were discovered in the middle of the last century and since then they have successfully dealt with numerous dangerous ailments.
Fluoroquinolones against bacteria
A modern person is constantly exposed to stress, numerous unfavorable environmental factors due to which his immune system malfunctions or weakens. In turn, pathogenic bacteria are constantly evolving, mutating, acquiring immunity to antibiotics of the penicillin series, which were successfully used to treat inflammatory diseases several decades ago. As a result, dangerous diseases quickly affect a person with a weakened immune system, and treatment with antibiotics of the old generation does not bring the desired results.
Bacteria are single-celled microorganisms that lack a nucleus. There are beneficial bacteria that are essential for the formation of human microflora. These include bifidobacteria, lactobacilli. At the same time, there are conditionally pathogenic microorganisms that, under concomitant conditions, become aggressive towards the body.
Scientists divide bacteria into 2 main groups:
- Gram positive.
These include staphylococci, streptococci, clostridia, corynebacteria, listeria. They cause the development of diseases of the nasopharynx, eyes, ears, lungs, bronchi.
- Gram negative.
These are Escherichia coli, Salmonella, Shigella, Moraxella, Klebsiella. They have a negative effect on the genitourinary system and intestines.
Based on this differentiation of the bacterial series, the doctor selects a therapy. If, as a result of bacterial inoculation, the causative agent of the disease is detected, then an antibiotic is prescribed that copes with the bacteria of this group. If the pathogen cannot be identified or it is impossible to conduct an analysis for bacterial culture, broad-spectrum antibiotics are prescribed, which have a detrimental effect on most pathogenic bacteria.
Classification
The broad spectrum antibiotics include the quinolone group, which includes fluoroquinolones, which destroy gram-positive and gram-negative bacteria, and non-fluorinated quinolones, which mainly destroy gram-negative bacteria.
The systematization of fluoroquinolones is based on the differences in chemical structure and spectrum of antibacterial activity. Fluoroquinolone antibiotics are divided into 4 generations according to the time of their development.
Includes nalidixic, oxolinic, pipemide acids. On the basis of nalidixic acid, uroantiseptics are produced, which have a detrimental effect on Klebsiella, Salmonella, Shigella, but cannot cope with gram-positive bacteria and anaerobes.
The first generation includes the drugs Gramurin, Negram, Nevigramon, Palin, the main active ingredient of which is nalidixic acid. It, like pipemidic and oxolinic acids, copes well with uncomplicated diseases of the genitourinary system and intestines (enterocolitis, dysentery). It is effective against enterobacteria, but it penetrates poorly into tissues, has a reduced bio-permeability, has many side effects, which makes it impossible to use non-fluorinated quinolones as a complex therapy.
Second generation.
Although the first generation of antibiotics had many shortcomings, it was recognized as promising and development in this area continued. After 20 years, the next generation of drugs have been developed. They were synthesized by introducing fluorine atoms into a quinoline molecule. The effectiveness of these drugs directly depends on the number of introduced fluorine atoms and their localization in different positions of quinoline atoms.
This generation of fluoroquinolones consists of Pefloxacin, Lomefloxacin, Ciprofloxacin, Norfloxacin. They destroy a greater number of gram-negative cocci and rods, fight against gram-positive rods, staphylococci, suppress the activity of fungal bacteria that contribute to the development of tuberculosis, but do not effectively fight anaerobes, mycoplasmas, chlamydia, pneumococci.
Third generation.
The main development goal that scientists pursued when creating antibiotics was achieved by the second generation of fluoroquinolones. With their help, you can fight especially dangerous bacteria, curing patients from life-threatening pathologies. But the development continued and soon there were drugs of the 3rd and 4th generations.
Respiratory fluoroquinolones, which have proven to be effective in the treatment of respiratory diseases, belong to the 3rd generation. They are much more effective in fighting chlamydia, mycoplasma and other pathogens of respiratory diseases than their predecessors, and have a wide range of effects. They are active against pneumococci, which have developed resistance to penicillin, which guarantees success in the treatment of bronchitis, sinusitis, pneumonia. The most commonly used are Levofloxacin, as well as Temafloxacin, Sparfloxacin. The bioavailability of these drugs is 100%, so they can be used to treat the most severe diseases.
Fourth generation or anti-anaerobic respiratory fluoroquinolones.
The drugs are similar in their action to fluoroquinolones - antibiotics of the previous group. They act against anaerobes, atypical bacteria, macrolides, penicillin-resistant pneumococci. They help well in the treatment of the upper and lower respiratory tract, inflammatory processes of the skin and soft tissues. The latest generation of drugs include Moxifloxacin aka Avelox, which is most effective against pneumococci, an atypical pathogenic microorganism, but not very effective against gram-negative intestinal microorganisms and Pseudomonas aeruginosa.
The drugs include Grepofloxacin, Clinofloxacin, Trovafloxacin. But they are highly toxic and have a lot of side effects. Currently, the last 3 types of drugs are not used in medicine.
Advantages and disadvantages of fluoroquinolones
Medicines containing fluoroquinolones find their place in various fields of medicine. The list of diseases that are treated with fluoroquinol antibiotics is very wide. They are used in gynecology, venereology, urology, gastroenterology, ophthalmology, dermatology, otolaryngology, therapy, nephrology, pulmonology. Also, these drugs are the best choice when macrolides and penicillins are ineffective or in case of severe forms of the disease.
They are characterized by the following properties:
- high results in the fight against systemic infections of all severity;
- easy tolerance by the body;
- minimal side effects;
- effective against gram-positive, gram-negative bacteria, anaerobes, mycoplasmas, chlamydia;
- the half-life is long;
- high bioavailability (they penetrate well into all tissues and organs, providing a powerful therapeutic effect).
Despite the effectiveness of fluoroquinolone antibiotics, when choosing a therapy, it should be borne in mind that they have contraindications for use. They are prohibited during pregnancy and breastfeeding, as they cause intrauterine malformations in the fetus, and hydrocephalus in infants. In babies, fluoroquinolones slow down bone growth, so they are prescribed only if the benefits of antibiotic therapy outweigh the harm to the child's body. Oxolinic and nalidixic acids have a toxic effect on the kidneys, therefore drugs with them are prohibited for kidney problems.
Applications
Antibiotics of the fluoroquinolone group rightfully occupy a leading position in the treatment of pathologies caused by pathogenic bacteria. They have a high degree of bioactivity, are well tolerated by humans, perfectly penetrate the bacterial membrane, and create protective substances in the cell that are close in concentration to serums.
The list of medications and the names of drugs that contain fluoroquinolones, their effectiveness is discussed below.
Ciprofloxacin. Designed for the treatment of ENT diseases, organs of the genitourinary system, gastrointestinal tract. Effective for gynecological problems. It is used in the form of drops for inflammatory eye diseases.
Pefloxacin. Effective in the treatment of infectious diseases of the urinary system. It helps well with gonorrhea, bacterial prostatitis. Treats severe forms of diseases of the gastrointestinal tract, throat, lower respiratory tract, nasopharynx.
Ofloxacin. Effective against pathogenic microorganisms causing inflammation in the urinary tract, otitis media, sinusitis. With the help of Ofloxacin, meningitis, chlamydia, and gonorrhea are treated. In a drop form, the antibiotic is used to treat eye diseases such as corneal ulcers, conjunctivitis, and barley. The medicine is also available in the form of an ointment, which allows it to be applied topically.
Norfloxacin. It is used in the treatment of gonorrhea, prostatitis, diseases of the genitourinary system.
Ofloxacin. Effective against chlamydia, pneumococcus and resistant forms of tuberculosis.
Moxifloxacin. The antibiotic is the best when it comes to eliminating the infection caused by mycoplasmas, chlamydia, pneumococci, anaerobes. It is used for pneumonia, sinusitis, inflammation of the pelvic organs. In liquid form (drops), it is used by ophthalmologists in the treatment of blepharitis, corneal ulcer, barley.
Gatifloxacin. It is used in the treatment of cystic fibrosis, bronchitis, pneumonia, conjunctivitis caused by bacterial infection, ENT diseases, diseases of the joints, skin.
Hemifloxacin. They are treated with sinusitis, chronic bronchitis, pneumonia.
Sparfloxacin. It fights very actively and effectively against mycobacteria, while its effect lasts much longer than that of other fluoroquinolones. It is used to treat diseases associated with inflammation of the middle ear, maxillary sinuses, infections of the kidneys, skin and soft tissues, reproductive and urinary systems, gastrointestinal tract, joints and bones.
Levofloxacin. Used for the treatment of infectious ENT diseases, lower respiratory system, genitourinary organs, STDs, acute pyelonephritis, chronic prostatitis. For eye infections, Levofloxacin is used in the form of drops. The antibiotic is twice as strong and powerful in fighting pathogenic bacteria, while better tolerated by the body than its predecessor Ofloxacin.
Norfloxacin. It is used as the main drug in gynecology, ophthalmology, urology.
Lomefloxacin. An antibiotic, even in small concentrations, copes with a large percentage of bacterial microorganisms by 5. It is prescribed in the presence of diseases of the genitourinary system, tuberculosis, as a local remedy for eye diseases. Ineffective for combating chlamydia, pneumococcus, mycoplasma.
IMPORTANT! Some fluoroquinolones (Sparfloxacin, Gatifloxacin, Ofloxacin, Moxifloxacin, Levofloxacin, Ciprofloxacin, Lomefloxacin) are included in the list of essential medicines approved by the Government of the Russian Federation.
For a long time, the specific chemical structure of fluoroquinolones did not allow obtaining liquid medicines with their use, so they were produced only in tablets. In the modern pharmaceutical industry there is a huge selection of ointments, drops and other varieties of antimicrobial drugs containing fluoroquinolones. This allows you to effectively fight deadly diseases of a bacterial nature.
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